neprilysin

Racecadotril (Acetorphan) has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis.

Sacubitril/Valsartan (LCZ696) is an orally bioavailable, dual angiotensin II receptor and neprilysin inhibitor for the treatment of hypertension and heart failure.

Sacubitril hemicalcium salt (AHU377 calcium salt) is a potent NEP inhibitor with an IC50 of 5 nM. Sacubitril hemicalcium salt is a component of the heart failure medicine LCZ696. Sacubitril hemicalcium salt is a prodrug of LBQ657, which is an inhibitor of the zinc metallopeptidase neprilysin. Neprilysin degrades a variety of vasoactive peptides such as atrial and brain natriuretic peptide, bradykinin, adrenomedullin, and endothelin-1. Inhibition of neprilysin leads to an increased level of these peptides and, thus, antihypertensive effects. Formulations containing AHU377 in combination with the angiotensin II receptor antagonist valsartan are used to treat hypertension and heart failure.

Sacubitril (AHU-377) is a potent NEP inhibitor with an IC50 of 5 nM and is a component of the heart failure medicine LCZ696.

Phosphoramidon Disodium (Phosphoramidon Disodium Salt) Salt is a metalloendopeptidase inhibitor, widely used as a biochemical tool.

Thiorphan is an neprilysin inhibitor (NEP; IC50 : 0.007 μM).

Sacubitrilat (LBQ-657) (LBQ657) is an effective inhibitor of active neprilysin (NEP).

Candoxatril (UK 79300) is an orally active neutral peptide endonuclease (NEP, EC 3.4.24.11) inhibitor that improves exercise capacity in patients with chronic heart failure undergoing angiotensin-converting enzyme inhibition.

NEP-IN-1 is an inhibitor of neutral endopeptidase (NEP, IC50 = 2 nM) and can be used in studies about female sexual arousal disorders.

Sacubitril sodium (AHU-377) is a potent NEP inhibitor with an IC50=5 nM for the treatment of heart failure or in combination with antihypertensive agents.

TD-0212 is an orally active dual pharmacology antagonist of angiotensin II type 1 receptor (AT1) and inhibitor of neprilysin (NEP)(pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP).

TD-0212 TFA is an orally active dual pharmacology compound, functioning as an antagonist of the angiotensin II type 1 receptor (AT1) with a pKi of 8.9, and as an inhibitor of neprilysin (NEP) with a pIC50 of 9.2.

Racecadotril-d5 is intended for use as an internal standard for the quantification of racecadotril by GC- or LC-MS. Racecadotril is a prodrug form of the neprilysin (NEP) inhibitor thiorphan. In vivo, racecadotril reduces or prevents castor oil-induced diarrhea without delaying intestinal transit in rats when administered at doses of 80 or 100 mg/kg, respectively. It also decreases the duration of diarrhea and increases body weight gain in a neonatal gnotobiotic pig model of human rotavirus-induced diarrhea. Formulations containing racecadotril have been used in the treatment of acute diarrhea.

SCH 42495 is an orally active neutral metalloendopeptidase inhibitor and serves as the ethyl ester prodrug of SCH 42354.

SCH 42495 racemate is the racemate of SCH 42495, an orally active neutral inhibitor of metalloendopeptidase (NEP) with antihypertensive effects.

SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP).

NEP-IN-2 is a neutral endopeptidase inhibitor used in the research of proliferation in atherosclerosis and restenosis.

Sampatrilat is an effecive and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase. Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM).

LHW090-A7 is an neutral endopeptidase (NEP) inhibitor, and an enzyme responsible for the metabolic inactivation of enkephalins.

JA2 is an inhibitor of metalloendopeptidase 24.15 that enhances the hypotensive response to bradykinin in rats.

Phosphoramidon is a membrane metallo-endopeptidase & endothelin-converting enzyme inhibitor and thermolysin inhibitor, which is obtained from culture filtrate of Streptomyces tanashiensis.

SDUY817 is a dual APN NEP inhibitor with IC50 values of 0.29 μM for APN and 7.4 μM for NEP. It exhibits analgesic effects in a concentration- and time-dependent manner, making it a potential candidate for research in the field of neuropathic pain disorders.

SDUY816 is an orally active dual APN NEP inhibitor, with IC50 values of 0.68 μM for APN and 6.9 μM for NEP. It exhibits analgesic properties and demonstrates good safety and pharmacokinetic profiles, having an oral bioavailability of 27% and a half-life of 4.02 hours in rats (oral, 10 mg kg). SDUY816 is applicable for research in the field of neuropathic pain disorders.

Antidiabetic agent 15 (compound 1B15) acts as a dual inhibitor of AT1R and NEP, reducing oxidative stress and restoring mitochondrial membrane potential.